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Aqueous based capsaicinoid formulations and methods of manufacture and use

一种辣椒素、辣椒碱的技术，应用在抗炎剂、医药配方、非中枢性止痛剂等方向

Inactive Publication Date: 2016-09-21
PREPA THERAPEUTICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is an unmet need for safe and effective therapies for the treatment of chronic pain

Method used

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  • Aqueous based capsaicinoid formulations and methods of manufacture and use
  • Aqueous based capsaicinoid formulations and methods of manufacture and use
  • Aqueous based capsaicinoid formulations and methods of manufacture and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0172] Preparation of concentrated capsaicin / PS 80 solution

[0173] US Patent 8637569 teaches that 5 mg / ml of PS 80 is required to dissolve 1 mg / ml of capsaicin, ie to obtain a capsaicin concentration of 0.06 mg / ml, only 0.3 gm / ml of PS 80 is required. Furthermore, it was determined that the relatively water-insoluble capsaicin contained in the micelles required 5 mg / ml of PS 80 for every 1 mg / ml increase in capsaicin solubility. The teaching of this patent was used in solubilizing capsaicin in high purity PS80 from Croda Corporation. .

[0174] Step I – Preparation of Capsaicin and PS 80 Concentrate

[0175] Ingredients include:

[0176] 10 grams of Polysorbate 80 (PS 80), Superfine, Croda, CAS#9005-65-6

[0177] 2 grams of trans-capsaicin, Aversion Technologies, USP 30, 95.7% trans-capsaicin, balanced cis-capsaicin

[0178] program:

[0179] 1. Add 10 grams of PS 80 to a 50ml "Pyrex" glass vial.

[0180] 2. Add 2 grams of trans-capsaicin to the PS 80 in step 1.

...

Embodiment 2

[0185] Preparation of 200 grams of aqueous solution containing capsaicin / PS80 concentrate and hyaluronic acid from Example 1

[0186] Step 1 - Preparation of Hyaluronic Acid Solution

[0187] Ingredients include:

[0188] 1 gram of hyaluronic acid, M.W. = 1000 kilodaltons, Lotioncrafter LLC, CAS#9067-32-7

[0189] 191.8 grams of distilled water, Poland Springs

[0190] program:

[0191] 1. Add 1 gram of Hyaluronic Acid to a 400cc Pyrex beaker.

[0192] 2. Add 191.8 grams of water to the hyaluronic acid and mix well until a clear solution is obtained. It takes longer to completely dissolve hyaluronic acid.

[0193] Step II - Preparation of 0.6mg / ml capsaicin, 3.0mg / ml PS80 & 5mg / ml hyaluronic acid aqueous solution

[0194] Ingredients include:

[0195] 7.2 grams of capsaicin / PS 80 concentrate from Example 1

[0196] 192.8 grams of hyaluronic acid from step I.

[0197] program:

[0198] 1. To the 192.8 grams of hyaluronic acid solution prepared in step I and containe...

Embodiment 3

[0204] Preparation of 200 g of 0.06 mg / ml capsaicin injectable solution (without micelles)

[0205] Step I - Preparation of Capsaicin, Phenol, Menthol Solution

[0206] Ingredients include:

[0207] 60 grams of PEG-300, Spectrum Chemical, NF, CAS#25322-68-3

[0208] 16 grams of ethanol, Graves Grain Alcohol, 190Proof

[0209] 0.2 grams of phenol, liquefied (phenolic acid), Spectrum Chemical, USP, CAS# 108-95-2

[0210] 0.2 g of L-menthol, crystalline, Spectrum Chemical, USP, CAS# 2216-51-5

[0211] 0.012 g of trans-capsaicin, Aversion Technologies, USP 30, 95.7% trans-capsaicin, balanced cis-capsaicin

[0212] program:

[0213] 1. Add 60 grams of PEG-300 to a 400cc Pyrex beaker.

[0214] 2. Add 16 grams of ethanol to the PEG-300 and mix well.

[0215] 3. Add 0.2 grams of liquefied phenol to the mixture from step 2.

[0216] 4. Add 0.2 grams of L-menthol crystals to the mixture from step 3.

[0217] 5. Add 0.012 grams of trans-capsaicin to the mixture from step 4.

...

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PUM

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Abstract

The invention discloses capsaicinoid formulations and methods of treatment are disclosed herein which can be utilized to treat / attenuate pain in mammals. Typically, administration is via injection at a discrete site to provide pain relief for an extended period of time. The formulations are administered in a pharmaceutically acceptable vehicle. The formulations include an analgesic agent in an amount sufficient to attenuate the burning and hyperalgesic effects of capsaicinoid administration. The invention also includes a method of treating pain by administering a corticosteroid followed by administration of a capsaicinoid.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of priority from US Application No. 14 / 078,253, filed November 12, 2013, the entire contents of which are expressly incorporated herein by reference. technical field [0003] The present invention relates to compositions for topical application of capsaicin. The compositions are useful in the treatment of a variety of disorders involving pain (acute and chronic, mild to severe), and they provide prolonged pain relief. The present invention also relates to methods comprising pre-treatments that limit the burning and stinging pain associated with capsaicin injections. Background technique [0004] Capsaicin, a pungent substance in the fruit of capsicum, has a relieving effect on pain caused by localized degeneration of C nerve endings; capsaicin is the only analgesic known to relieve pain by this mechanism. The activity of capsaicin results from its binding to and activation of an i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/165
CPCA61K9/0019A61K45/06A61K31/085A61K31/167A61K31/728A61K9/0024A61K47/36A61K31/165A61K31/05A61K31/045A61P17/02A61P19/02A61P25/04A61P29/00A61P43/00A61K2300/00A61K9/08A61K47/10A61K47/26
Inventor 查尔斯·A·比尔巴拉菲利普·J·比尔巴拉丹尼尔·巴克斯玛丽·库格林
Owner PREPA THERAPEUTICS CO LTD
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